1. Field of the Invention
The present invention relates to a new 9-aminoacridine derivative of the general formula (I)
wherein Y is a bond or
(wherein X is oxygen or sulfur, R1, R2, R3, R4 and R5 are independently hydrogen, halogen, nitro, amino, hydroxy, C1–C4 lower alkylhydroxy, C1–C4 lower alkoxy, R′ and R″ are independently C1–C4 alkyl or C1–C4 lower alkoxy, and Z is C1–C4 lower alkyl, C1–C4 lower alkoxy or C1–C4 lower alkylamino.
In the above definitions, C1–C4 lower alkyl means straight or branched alkyl groups such as methyl, ethyl, propyl, isopropyl, n-butyl, isobutyl, sec-butyl or the like.
C1–C4 lower alkoxy means methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy, tert-butoxy or the like.
C1–C4 lower alkylamino means methylamino, ethylamino, propylamino, butylamino or the like.
2. Description of the Prior Art
WO 00/37447 describes 9-amnoacridine derivatives and process for the preparation thereof of the compounds of the formula (1)
wherein A is hydrogen or
(wherein X is oxygen or sulfur, R1, R2, R3, R4 and R5 are independently hydrogen, halogen, nitro, amino, hydroxy, C1–C4 lower alkylhydroxy, C1–C4 lower alkylamino, C1–C8 alkyl, C1–C4 lower alkoxy or C1–C4 lower alkyloxycarbonyl and m and n are independently an integer of 0, 1 or 2.), R6, R7, R8 and R9 are independently C1–C8 alkyl or C1–C4 lower alkoxy, and Y is hydrogen, amino, —N═CHR′ (wherein R′ is hydrogen, benzyl, C1–C8 alkyl or C1–C6 lower alamino),
(wherein R″ is hydrogen, benzyl, C1–C8 alkyl or C1–C6 lower alkylamino, and R′″ is hydrogen, benzyl, C1–C8 alkyl or amino protecting group) or
(wherein, X is as defined above, R1′, R2′, R3′, R4′ and R5′ are independently hydrogen, halogen, nitro, amino, hydroxy, C1–C4 lower alkylhydroxy, C1–C4 lower alkylamino, C1–C8 alkyl, C1–C4 lower alkoxy or C1–C4 lower alkyloxycarbonyl, and q and r are independently an integer of 0, 1 or 2) or its pharmaceutically acceptable salt, and process for the preparation thereof.
In the above compounds of the formula (I) wherein Y is
(R″ and R′″ are as defined above.), there may be isomers of l-form, d-form or racemic form.
However, the compound of the present invention does not describe in the WO 00/37447.